How harmful is tramadol abuse – what’s it really doing in
your body and are you going to suffer long-term physical health consequences from
your habit?

If you’re a chronic user, you’ve probably wondered about the
dangers, so read on to learn more about what tramadol does in your brain and
body and about the health risks associated with acute and chronic use, specifically:

How tramadol works in the brain.

Tramadol’s addiction potential and how it compares to drugs
like oxycodone.

Seizure risks and what exacerbates these risks.

Overdose signs and treatments.

Serotonin syndrome signs and treatments.

Tramadol and neonatal abstinence syndrome.

Tramadol’s effects on sleep, its negligible cancer profile
and the potential for organ damage.

How Does Tramadol Work in the Brain?

Though reading the complex neuroscience behind tramadol
can be tough slogging, it’s a good idea to gain at least a basic idea of what it’s
doing in your brain. Here's a very brief overview of the
medication's 2 primary modes of action.

Disconcertingly, scientists don’t have a total understanding
of how tramadol works. Consider this quote from the medication insert, “Tramadol
hydrochloride is a centrally acting synthetic opioid analgesic. Although its
mode of action is not completely understood.” !!! 1

But here’s what is known:

Tramadol influences 2
primary brain systems:

The opioid system - by binding with u-opioid receptors.

the monoamine system - by inhibiting the reuptake of serotonin and norepinephrine.

Tramadol is partially metabolized in the liver by the
enzymes CYP2D6 and CYP3A4. The tramadol metabolized by CYP2D6 becomes a
substance called O-Desmethyltramadol. Both the original tramadol compound
and O-Desmethyltramadol stimulate u-opioid receptors in the brain, though
the O-Desmethyltramadol has 6 times the affinity for these receptors than the original compound.

For analgesia (and intoxication) both the opioid
and serotonin/norepinephrine systems are important. We know this becasue blocking opioid receptor
activation with naloxone does not completely eliminate analgesia or abuse
potential.

The Acute and Chronic Risks of Tramadol Abuse

Though tramadol isn't as risky or harmful as full-agonist opiates, with short or long-term abuse you are at risk of some serious health consequences.

Addiction

If you take tramadol chronically you will develop a physical
dependence and will experience withdrawal symptoms should you stop
taking the drug too suddenly.

You are also at risk of addiction, which is distinct from
physical dependence - especially if you ever take more tramadol than prescribed for pain management or if you ever take tramadol just to feel good.

Symptoms of Tramadol Addiction Include:

A loss of control over your tramadol use (for example, being
unable to manage your supply of medication to last between prescriptions).

Compulsive use.

Using tramadol for non-medical reasons (to get high).

Continuing to use tramadol despite being aware that it does
you harm or risks you harm (examples could include excessive financial harms,
risks of overdose, a failure to meet responsibilities, legal problems, etc.)

Tramadol was originally touted as a drug with significantly
less abuse and addiction potential than comparable full-agonist opioids. While
it’s still considered less addictive than full-opioids, the FDA now acknowledges
tramadol’s abuse risk and advises against prescribing this drug to people considered
addiction prone or those who use alcohol to excess.

Study: Comparing Tramadol’s Abuse Risk to Oxycodone’s

In a study of abuse potential, researchers at the University
of Kentucky College of Medicine compared tramadol, codeine, oxycodone and a
placebo to see how much drug abusers liked each substance (they didn’t know
what they were taking) and to see how hard they would work for further doses.

For the study:

All subjects were non opiate-dependent recreational opiate
abusers.

To test the 3 different drugs, all subjects came in for 7
times for 2-day experimental procedures. On each day 1, researchers gave each subject one of
the 4 substances; the subjects then rated this drug for recreational likeability and learned they’d be
working the next day to earn doses of this substance.

On each day 2, subjects came back in and worked (through button
clicking exercises) to earn small doses of the same drug.

The Results:

Subjects did not like the placebo and would not work for it.

On a scale to 100, when rating how much they liked the pleasurable high,
subjects gave 40 mg of oxycodone a score of a little more than 62, 200 mg of
codeine a score of 49 and 400 mg of tramadol a score of 47.

Though subjects reported liking the oxycodone high more than
the tramadol high, subjects were willing to work harder to get more tramadol
than they were to get more oxycodone or codeine.3

The Significant Risks of Seizure

High dose tramadol abuse is associated with a significant
risk of seizure. Consider the following studies which illustrate the dangers.

The Belgrade Study

Researchers at Belgrade University Medical School followed a
group of 57 tramadol abusers/addicts over a three year period.

Over that three year period, 31 subjects (54%) had at least
one serious seizure – 17 of them had multiple seizures over that period and
14 had a single seizure.

Doses prompting seizures ranged from 250 mg to 2500 mg and
the vast majority of seizures occurred within 24 hours of acute intoxication.

Factors that increased the risk of seizure
included: a longer history of tramadol abuse, younger age and the concurrent
use of alcohol.4

The Baghdad Study

Out of 41
patients referred to the addiction unit of the Ibn-Rushed Mental Teaching
Hospital, 20% had experienced at least one tramadol related seizure.5

The Iran Study

And in a review
of cases from Baharloo Hospital Poison Center in Iran, out of 401 patients
admitted for tramadol overdose, 30.2% reported a history of seizures.6

Who Is Most at Risk of Seizure?

People who take more than the recommended daily dose of
tramadol are at greater risk of seizures (though seizures can occur within the
recommended dosing range). You are also at higher risk of tramadol-induced
seizures if you are/have:

Managing Tramadol Seizures

Tramadol seizures can be managed with diazepam (Valium).

Overdose: Symptoms and Treatments

Tramadol can be lethal in very high doses. For adults, the
estimated lethal dose ranges from between 3 and 5 grams.8 The lethal dose is lowered when taking tramadol concurrently with other CNS
depressants, like alcohol or other sedatives, and overdose deaths have occurred
from combinations of CNS depressants and tramadol.9

Most of the toxicity associated with tramadol overdose stems from excessive serotonin, and norepinephrine reuptake
inhibition…too much tramadol results in too much serotonin and norepinephrine
in the brain.

Serotonin Syndrome

If you take tramadol together with another drug that also
increases serotonin levels, like SSRI/SNRIs, MAOIs, dextromethorphan (a cough
syrup ingredient), Demerol and others - or with illicit drugs like MDMA or LSD,
you risk bumping your serotonin to dangerous levels and experiencing a possibly
lethal condition known as serotonin syndrome.

During slow wave sleep blood flows away from the brain and
into muscle tissue, the body builds muscle and bone, the immune system is
strengthened and the body repairs damaged tissues, such as those damaged by
ultraviolet rays.

Areas of the brain which control emotion, decision making and
social functioning go dormant. Sleep scientists
think this decreased activation while sleeping helps us maintain maximal social
attention and functioning while awake.

Of course, everything depends on your individual situation. For
example, if tramadol provides analgesia that increases sleep likelihood, it may
have a net-positive impact on sleep quality and quantity.

Cancer and Organ Damage

There is no evidence from animal-model studies that chronic
tramadol use increases human cancer risk.

Because tramadol is not associated with an increased cancer
risk, or with gastrointestinal, renal or cardiovascular complications, it is
considered an appropriate (safe) medication for chronic pain treatment.15

It is not, however, totally benign. Researchers who compared the long
term use of tramadol to morphine in an animal-model study concluded that though
tramadol was far less toxic to the liver and kidneys than morphine, it still
did some damage over time.16

Use during Pregnancy/Nursing

Tramadol may slightly increase birth defect risks if used during the first 2 months of pregnancy.

If used during pregnancy, especially chronically
or in high doses close to the expected date of delivery, the baby may be born
with neonatal abstinence syndrome (NAS).17

Tramadol is passed through breast milk to your infant. Talk
to your doctor before using tramadol while nursing.18

Those creepy-crawly-jumpy legs that make sleep impossible – there are few things worse than the restless legs of opiate withdrawal. Only time will solve the problem, but there are medications and home-remedy treatments that can minimize their severity. Read on to get the tips you need to get to sleep. Read Article